Cap-dependent endonuclease-IN-3 is a potent inhibitor of cap-dependent endonuclease (CEN). Not only can Cap-dependent endonuclease-IN-3 inhibit influenza virus well, but also has lower cytotoxicity, better in vivo agent kinetic properties and in vivo pharmacodynamic properties. Cap-dependent endonuclease-IN-3 has the potential for the research of influenza A and influenza B infection (extracted from patent WO2019141179A1, compound VI-1)[1].
Glyceryl 1-monooctanoate is a glycerol monolaurate derivative. Glyceryl 1-monooctanoate is a broad-spectrum antimicrobial, suppresses the growth of pathogenic yeast (Candida albicans and Candida parapsilosis), as well as Gram-positive (Staphylococcus aureus) and Gram-negative (Escherichia coli, Klebsiella pneumoniae) bacteria[1].
Methyl salvionolate A is a potent inhibitor of HIV-1. Methyl salvionolate A inhibits P24 antigen in HIV-1 infected MT-4 cell with an EC50 of 1.62 μg/ml. Methyl salvionolate A also inhibits HIV-1 reverse transcriptase, protease and integrase with IC50s of 50.58, 10.73 and 7.58 μg/ml, respectively[1].
Temporin G is an antimicrobial peptide against Legionella pneumophila[1].
SQ609 is a lead compound from a library of dipiperidines. SQ609 inhibits more than 90% of intracellular bacterial growth at 4μg/ml and is toxic to these cells. SQ609 displays a potent antitubercular activity [1].
CHIR-090 is a potent, slow, tight-binding inhibitor of the LpxC deacetylase. It binds to E. coli LpxC with a Ki of 4.0 nM.
Ceftibuten (Sch39720) hydrate, an antibiotic, is an orally active cephalosporin, possesses potent activity in vitro against a wide range of gram-negative and certain gram-positive pathogens[1][2].
Prulifloxacin(NM441) is an older synthetic antibiotic of the fluoroquinolone drug class.Target: AntibacterialPrulifloxacin prevents bacterial DNA replication, transcription, repair and recombination through inhibition of bacterial DNA gyrase.
(2RS)-FPMPA can be used for synthesis of antiretroviral agents against HIV-1 and HIV-2[1].
Enterocin, an antibiotic, has static activities against gram-positive and gram-negative bacteria and no activity against fungi and yeast[1].
Rifamycin (Rifamycin SV) belongs to the family of ansamycin antibiotics and has been isolated from the fermentation of A. mediterranei or its mutants. Rifamycin displays a broad spectrum of antibiotic activity against Gram-positive and, to a lesser extent, Gram-negative bacteria[1].
Neuraminidase-IN-10 is a potent neuraminidase (NA) inhibitor with anti-influenza activity. Neuraminidase-IN-10 is against H1N1, H5N1, and H5N8 with IC50 values of 2.6 nM, 5.1 nM, and 1.65 nM, respectively[1].
Emtricitabine Degradant-III is a major degradation product of Emtricitabine. Emtricitabine is a potent nucleoside reverse transcriptase inhibitor used for the treatment of HIV infection.
LY 215890 ia an orally active antibacterial agent aganist Escherichia coli EC14 and Klebsiella pneumonia X26[1].
Cefozopran(SCE 2787) is a fourth-generation cephalosporin.Target: AntibacterialCefozopran is a fourth-generation cephalosporin.
Azlocillin is an acylampicillin with a broad spectrum against bacteria.Target: AntibacterialAzlocillin (12.5 μg/mL) inhibits over 75% of the isolates of Pseudomonas aeruginosa. Azlocillin (12.5 μg/mL) is also active against indole-negative and -positive Proteus spp., inhibiting 98 and 71%, respectively. Azlocillin is more active than mezlocillin, ticarcillin, and carbenicillin and as active as BLP-1654 against isolates of P. aeruginosa [1]. The acyl side chains of Azlocillin have an ureido-(urea) structurehence the name "ureidopenicillins" or, more specifically, "acylureidopenicillins." In vitro studies against P. aeruginosa demonstrates that piperacillin has activity that is twice that of azlocillin, 4 times that of mezlocillin and ticarcillin, and about 8 times that of carbenicillin. Azlocillin produces elongated bacterial forms with delayed or no lysis in morphologic studies [2].Azlocillin has MICs of 12.5 μg/mL on Pseudomonas aeruginosa. Azlocillin (3.125 μg/mL) results in a reduction in the rate of growth but no bactericidal phase on Pseudomonas aeruginosa. Azlocillin decreases an initial lag phase with increasing drug concentration. At the lower concentration of tobramycin (0.5 μg/ml), the combinations with both the high and the low concentrations of Azlocillin are more effective than the individual components on Pseudomonas aeruginosa [3]. Isolates with derepression of AmpC enzyme are one to two doubling dilutions more resistant to azlocillin than are those in which increased efflux or impermeability is inferred. Those with secondary β-lactamases are mostly (12/14 cases) susceptible to ceftazidime at 4 mg/L, but are amongst the most resistant to Azlocillin (MIC ≥128 mg/L in 10/14 cases) [4].
GW779439X is a pyrazolopyridazine identified in an inhibitor of the S. aureus PASTA kinase Stk1. GW779439X potentiates the activity of β-lactam antibiotics against various MRSA and MSSA isolates, some even crossing the breakpoint from resistant to sensitive. GW779439X is an AURKA inhibitor and induces apoptosis by the caspases 3/7 pathway[1][2]. MRSA:methicillin-resistant S. aureus; MSSA: methicillin-sensitive S. aureus
Hepcidin-20 (human) is a histidine-containing, cysteine-rich, β-sheet structured peptide. Hepcidin-20 (human) shows antifungal activity. Hepcidin-20 (human) inhibits biofilm formation and bacterial cell metabolism of polysaccharide intercellular adhesin (PIA)-positive and PIA-negative strains[1][2][3].
Gramicidin is an antimicrobial peptide assembling as channels in membranes and increasing their permeability towards cations.
Celgosivir hydrochloride (MDL 28574A) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
Glycosmisic acid, a natural compound, possesses anti-HBV activity[1].
(S)-Tedizolid is the S-enantiomer of Tedizolid. Tedizolid is a novel oxazolidinone with activity against Gram-positive pathogens. (S)-Tedizolid is the less active isomer.
Penamecillin (Wy 20788) an acetoxymethyl ester of Penicillin G (HY-N7139). Penamecillin is an orally active antibacterial agent[1][2].
Eckol is a potent hMAO-A (Mixed) and hMAO-B (non-competitive) inhibitor with IC50s of 7.20 and 83.44 μM, respectively. Eckol shows stimulatory effects in maize and can be used as a plant biostimulant. Eckol also shows antiallergic and antiviral effects[1][2][3][4].
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties[1][2][3][4].
Zevotrelvir (Compound 52) is a coronavirus inhibitor with IC50 ranges of <0.1 μM and <0.1mM for 229E hCoV and SARS-CoV-23C-like (3CL) proteases, respectively. Zevotrelvir has the potential to study viral infections[1].
Aztreonam (lysine) is a monocyclic beta-lactam antibiotic, and has a very high affinity for penicillin-binding protein 3 (PBP-3). Aztreonam (lysine) is active against Gram-negative aerobic bacteria[1][2].
Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors[1].
Panipenem (PAPM; CS533; RS533) is a carbapenem antibiotic with broad spectrum and potent activity against both Gram-positive and Gram-negative bacteria[1].